2. Academic Validation
  3. A novel atypical retinoid endowed with proapoptotic and antitumor activity

A novel atypical retinoid endowed with proapoptotic and antitumor activity

  • J Med Chem. 2003 Mar 13;46(6):909-12. doi: 10.1021/jm025593y.
Raffaella Cincinelli 1,  Sabrina Dallavalle,  Lucio Merlini,  Sergio Penco,  Claudio Pisano,  Paolo Carminati,  Giuseppe Giannini,  Loredana Vesci,  Carlo Gaetano,  Barbara Illy,  Valentina Zuco,  Rosanna Supino,  Franco Zunino
Affiliations

Affiliation

  • 1 Dipartimento di Scienze Molecolari Agroalimentari, Università di Milano, Milano, Italy.
PMID: 12620066 DOI: 10.1021/jm025593y
Abstract

The novel atypical retinoid E-3-(4'-hydroxy-3'-adamantylbiphenyl-4-yl)acrylic acid (ST1926, 4) exhibited a potent antiproliferative activity on a large panel of human tumor cells. Despite almost complete loss of ability to activate RARs, the compound was an effective Apoptosis inducer and surprisingly produced DNA damage, that likely contributes to the proapoptotic activity. Following oral administration, 4 was well tolerated and caused tumor growth inhibition in the ovarian carcinoma, A2780/DX, and in the human melanoma, MeWo, growing in nude mice, thus supporting the therapeutic interest of the novel agent.

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